ganaplacide

Ganaplacide is an investigational small molecule antimalarial drug developed by Novartis for the treatment of malaria. It is an imidazolopiperazine derivative with activity against both *Plasmodium falciparum* and *Plasmodium vivax* parasites. Ganaplacide has demonstrated efficacy in clinical trials when combined with a new solid dispersion formulation of lumefantrine (lumefantrine-SDF), showing potential to clear malaria infections—including artemisinin-resistant strains—and block parasite transmission. The precise mechanism of action remains unknown; however, resistance studies indicate that mutations in the PfCARL protein (cyclic amine resistance locus), acetyl-CoA transporter (PfACT), and UDP-galactose transporter (PfUGT) can confer reduced susceptibility to ganaplacide. These proteins are believed to be involved in drug transport rather than being direct targets of the compound. Ganaplacide is being developed with support from Medicines for Malaria Venture and has received Fast Track and Orphan Drug Designation from the US FDA for use in combination therapy for acute uncomplicated malaria[1][4][5][6].

Other names

ganaplacide2-amino-1-[2-(4-fluorophenyl)-3-[(4-fluorophenyl)amino]-5,6-dihydro-8,8-dimethylimidazo[1,2-a]pyrazin-7(8H)-yl]ethanone